Bioactivity | Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively[1]. | ||||||||||||
Target | 640 nM (M2 muscarinic acetylcholine receptor in rabbit peripheral lung), 386 nM (M2 muscarinic acetylcholine receptor in rat heart). | ||||||||||||
In Vivo | Otenzepad (0.5, 1 mg/kg, s.c., in rats) significantly improved win-stay acquisition relative to vehicle-injected controls[2].Otenzepad (2 mg/kg, s.c., in rats) significantly improved retention relative to vehicle controls[2].Otenzepad (0.3, 1.0, or 3.0 mg/kg, ip, in mice) potentiates the effects of glucose and reverses the effects of insulin on memory[3]. Animal Model: | ||||||||||||
Name | Otenzepad | ||||||||||||
CAS | 102394-31-0 | ||||||||||||
Formula | C24H31N5O2 | ||||||||||||
Molar Mass | 421.54 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Bloom JW, et al. Heterogeneity of the M1 muscarinic receptor subtype between peripheral lung and cerebral cortex demonstrated by the selective antagonist AF-DX 116. Life Sci. 1987 Jul 27;41(4):491-6. [2]. Packard MG, et al. Post-training injection of the acetylcholine M2 receptor antagonist AF-DX 116 improves memory. Brain Res. 1990 Jul 30;524(1):72-6. [3]. Kopf SR, et al. AF-DX 116, a presynaptic muscarinic receptor antagonist, potentiates the effects of glucose and reverses the effects of insulin on memory. Neurobiol Learn Mem. 1998 Nov;70(3):305-13. |